IL149306A0 - Benzamidine derivatives and pharmaceutical compositions containing the same - Google Patents
Benzamidine derivatives and pharmaceutical compositions containing the sameInfo
- Publication number
- IL149306A0 IL149306A0 IL14930600A IL14930600A IL149306A0 IL 149306 A0 IL149306 A0 IL 149306A0 IL 14930600 A IL14930600 A IL 14930600A IL 14930600 A IL14930600 A IL 14930600A IL 149306 A0 IL149306 A0 IL 149306A0
- Authority
- IL
- Israel
- Prior art keywords
- group
- optionally substituted
- hydrogen atom
- alkyl group
- halogen atom
- Prior art date
Links
- 150000003937 benzamidines Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 208000015294 blood coagulation disease Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Manufacture Of Alloys Or Alloy Compounds (AREA)
Abstract
Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: <CHEM> wherein R<1> represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R<2> represents a hydrogen atom, a halogen atom or an alkyl group, R<3> represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R<4> and R<5> are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R<6> represents a substituted pyrrolidine group or substituted piperidine group.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP30719299 | 1999-10-28 | ||
| PCT/JP2000/007469 WO2001030756A1 (en) | 1999-10-28 | 2000-10-25 | Benzamidine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL149306A0 true IL149306A0 (en) | 2002-11-10 |
Family
ID=17966162
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL14930600A IL149306A0 (en) | 1999-10-28 | 2000-10-25 | Benzamidine derivatives and pharmaceutical compositions containing the same |
| IL149306A IL149306A (en) | 1999-10-28 | 2002-04-23 | Benzamidine derivatives and pharmaceutical compositions containing the same |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL149306A IL149306A (en) | 1999-10-28 | 2002-04-23 | Benzamidine derivatives and pharmaceutical compositions containing the same |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US6555556B1 (en) |
| EP (1) | EP1245564B1 (en) |
| KR (1) | KR100642953B1 (en) |
| CN (2) | CN1572882A (en) |
| AT (1) | ATE322479T1 (en) |
| AU (1) | AU776193B2 (en) |
| BR (1) | BR0015120A (en) |
| CA (1) | CA2389156C (en) |
| CY (1) | CY1106116T1 (en) |
| CZ (1) | CZ20021432A3 (en) |
| DE (1) | DE60027204T2 (en) |
| DK (1) | DK1245564T3 (en) |
| ES (1) | ES2261248T3 (en) |
| HK (1) | HK1047431B (en) |
| HU (1) | HUP0203161A3 (en) |
| IL (2) | IL149306A0 (en) |
| MX (1) | MXPA02004218A (en) |
| NO (1) | NO323147B1 (en) |
| NZ (1) | NZ518581A (en) |
| PL (1) | PL354619A1 (en) |
| PT (1) | PT1245564E (en) |
| RU (1) | RU2222529C2 (en) |
| TR (1) | TR200201654T2 (en) |
| TW (1) | TWI226886B (en) |
| WO (1) | WO2001030756A1 (en) |
| ZA (1) | ZA200203278B (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1572882A (en) * | 1999-10-28 | 2005-02-02 | 三共株式会社 | Benzamidine derivatives |
| PL363961A1 (en) * | 2001-04-05 | 2004-11-29 | Sankyo Company, Limited | Benzamidine derivative |
| WO2002089803A1 (en) * | 2001-05-07 | 2002-11-14 | Sankyo Company, Limited | Composition for iontophoresis |
| CA2479062A1 (en) * | 2002-03-15 | 2003-09-25 | Kissei Pharmaceutical Co., Ltd. | Novel crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative |
| CN101693029B (en) * | 2004-11-23 | 2011-11-02 | 同和药品（株） | Oral preparation having improved bioavailability |
| CN103159620A (en) * | 2013-03-28 | 2013-06-19 | 广西师范大学 | Preparation method of 2-hydroxyisophthalic acid |
| KR20250112249A (en) | 2022-11-22 | 2025-07-23 | 키메드 바이오사이언시스 (청두) 컴퍼니 리미티드 | Fused ring compounds, conjugates thereof and uses thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57209270A (en) * | 1981-06-19 | 1982-12-22 | Chugai Pharmaceut Co Ltd | Proline derivative |
| ZA928276B (en) | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
| US5731324A (en) * | 1993-07-22 | 1998-03-24 | Eli Lilly And Company | Glycoprotein IIb/IIIa antagonists |
| IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
| TW300888B (en) * | 1994-12-02 | 1997-03-21 | Yamanouchi Pharma Co Ltd | |
| DE4443390A1 (en) * | 1994-12-06 | 1996-06-13 | Basf Ag | New dipeptidic p-amidinobenzylamides with N-terminal sulfonyl or aminosulfonyl residues |
| SI9620136B (en) * | 1996-01-02 | 2005-08-31 | Aventis Pharma Inc | Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides |
| CA2264521A1 (en) * | 1996-09-12 | 1998-03-19 | Schering Aktiengesellschaft | Benzamidine derivatives substituted by cyclic amino acid or cyclic hydroxy acid derivatives and their use as anti-coagulants |
| TW542822B (en) | 1997-01-17 | 2003-07-21 | Ajinomoto Kk | Benzamidine derivatives |
| US6545054B1 (en) * | 1999-02-11 | 2003-04-08 | Millennium Pharmaceuticals, Inc. | Alkenyl and alkynyl compounds as inhibitors of factor Xa |
| US6350761B1 (en) * | 1999-07-30 | 2002-02-26 | Berlex Laboratories, Inc. | Benzenamine derivatives as anti-coagulants |
| CN1572882A (en) * | 1999-10-28 | 2005-02-02 | 三共株式会社 | Benzamidine derivatives |
-
2000
- 2000-10-25 CN CNA2004100634713A patent/CN1572882A/en active Pending
- 2000-10-25 CA CA002389156A patent/CA2389156C/en not_active Expired - Fee Related
- 2000-10-25 RU RU2002111343/04A patent/RU2222529C2/en not_active IP Right Cessation
- 2000-10-25 PT PT00970070T patent/PT1245564E/en unknown
- 2000-10-25 DK DK00970070T patent/DK1245564T3/en active
- 2000-10-25 AT AT00970070T patent/ATE322479T1/en not_active IP Right Cessation
- 2000-10-25 BR BR0015120-3A patent/BR0015120A/en not_active Application Discontinuation
- 2000-10-25 AU AU79574/00A patent/AU776193B2/en not_active Ceased
- 2000-10-25 DE DE60027204T patent/DE60027204T2/en not_active Expired - Lifetime
- 2000-10-25 IL IL14930600A patent/IL149306A0/en active IP Right Grant
- 2000-10-25 EP EP00970070A patent/EP1245564B1/en not_active Expired - Lifetime
- 2000-10-25 HK HK02108844.9A patent/HK1047431B/en not_active IP Right Cessation
- 2000-10-25 PL PL00354619A patent/PL354619A1/en unknown
- 2000-10-25 HU HU0203161A patent/HUP0203161A3/en unknown
- 2000-10-25 NZ NZ518581A patent/NZ518581A/en unknown
- 2000-10-25 CZ CZ20021432A patent/CZ20021432A3/en unknown
- 2000-10-25 MX MXPA02004218A patent/MXPA02004218A/en active IP Right Grant
- 2000-10-25 CN CNB008178003A patent/CN1293052C/en not_active Expired - Fee Related
- 2000-10-25 WO PCT/JP2000/007469 patent/WO2001030756A1/en not_active Ceased
- 2000-10-25 KR KR1020027005382A patent/KR100642953B1/en not_active Expired - Fee Related
- 2000-10-25 TR TR2002/01654T patent/TR200201654T2/en unknown
- 2000-10-25 ES ES00970070T patent/ES2261248T3/en not_active Expired - Lifetime
- 2000-10-27 TW TW089122706A patent/TWI226886B/en not_active IP Right Cessation
-
2002
- 2002-04-23 IL IL149306A patent/IL149306A/en not_active IP Right Cessation
- 2002-04-24 ZA ZA200203278A patent/ZA200203278B/en unknown
- 2002-04-25 US US10/132,042 patent/US6555556B1/en not_active Expired - Fee Related
- 2002-04-26 NO NO20021990A patent/NO323147B1/en not_active IP Right Cessation
- 2002-11-06 US US10/288,838 patent/US20040010009A1/en not_active Abandoned
-
2003
- 2003-11-07 US US10/704,355 patent/US20040248981A1/en not_active Abandoned
-
2006
- 2006-07-04 CY CY20061100927T patent/CY1106116T1/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed |